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A repaglinide crystal, its preparation method and solid oral preparation containing the crystal

A technology of oral preparations and crystals, which is applied in the field of medicine, can solve the problems of poor bioavailability and low solubility of repaglinide, and achieve the effect of convenient recycling, convenient separation and purification

Active Publication Date: 2011-12-07
HAINAN JINRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0016] Due to the low solubility and poor bioavailability of repaglinide, how to improve its dissolution rate is mainly considered in the design of the above prescription

Method used

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  • A repaglinide crystal, its preparation method and solid oral preparation containing the crystal
  • A repaglinide crystal, its preparation method and solid oral preparation containing the crystal
  • A repaglinide crystal, its preparation method and solid oral preparation containing the crystal

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] [Example 1] Preparation of repaglinide crystals

[0080] 1) Dissolve repaglinide powder in ethanol to prepare a repaglinide solution as the dispersed phase;

[0081] 2) Dissolve sodium 2-ethylhexyl succinate sulfonate in isooctane to prepare a sodium 2-ethylhexyl succinate sulfonate solution as a dispersion medium;

[0082] 3) Under an ultrasonic field, use a micro-injector to add the dispersed phase solution to the dispersion medium, continue to sonicate, and centrifuge to separate repaglinide ultrapowder, remove the supernatant and add isooctane to wash and centrifuge to remove Sodium 2-ethylhexyl succinate sulfonate adsorbed on the surface of repaglinide is dried in vacuum to obtain repaglinide crystals.

[0083] The particle size of the prepared repaglinide crystal is 1μm, and the X-ray powder diffraction pattern obtained by Cu-Kα ray measurement (see figure 1 The characteristic peaks in) are displayed at 2θ of 4.8°, 13.6°, 14.9°, 15.2°, 16.0°, 19.1°, 21.2° and 24.1°.

Embodiment 2

[0084] [Example 2] Preparation of repaglinide crystals

[0085] 1) Dissolve repaglinide powder in ethanol to prepare a repaglinide solution as the dispersed phase;

[0086] 2) Dissolve sodium 2-ethylhexyl succinate sulfonate in isooctane to make 0.05 mol·L -1 Sodium 2-ethylhexyl succinate sulfonate solution as the dispersion medium;

[0087] 3) In an ultrasonic field with a power of 0.1KW, use a micro-injector to add the dispersed phase solution to the dispersion medium, and continue to sonicate for 1 minute at 9000r·min -1 Repaglinide ultra-powder was separated by high-speed centrifugation under the conditions of high-speed centrifugation, and the supernatant was removed and isooctane washed and centrifuged twice to remove the sodium 2-ethylhexyl succinate sulfonate adsorbed on the surface of repaglinide. Vacuum drying for 8 hours, the repaglinide crystal is obtained.

[0088] The particle size of the obtained repaglinide crystal was 5 μm, and the X-ray powder diffraction pattern mea...

Embodiment 3

[0089] [Example 3] Preparation of repaglinide crystals

[0090] 1) Dissolve repaglinide powder in ethanol to prepare a repaglinide solution as the dispersed phase;

[0091] 2) Dissolve sodium 2-ethylhexyl succinate sulfonate in isooctane to prepare 0.3 mol·L -1 Sodium 2-ethylhexyl succinate sulfonate solution is used as the dispersion medium;

[0092] 3) In an ultrasonic field with a power of 0.3KW, add the dispersed phase solution to the dispersion medium with a micro-injector, and continue to sonicate for 3 minutes at 11000r·min -1 Repaglinide ultra-powder was separated by high-speed centrifugation under high-speed conditions, and the supernatant was removed and isooctane washed and centrifuged 4 times to remove the sodium 2-ethylhexyl succinate sulfonate adsorbed on the surface of repaglinide. After vacuum drying for 12 hours, repaglinide crystals were obtained.

[0093] The particle size of the obtained repaglinide crystal was 3 μm, and the X-ray powder diffraction pattern obtaine...

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Abstract

The invention relates to a repaglinide crystal, a preparation method thereof, and a solid oral preparation containing the same. The particle size of the crystal is 1 to 5 mu m. The solid oral preparation is a tablet prepared from repaglinide, compressible starch, microcrystalline cellulose calcium hydrogen phosphate, polyvinylpyrrolidone, cross-linked sodium carboxymethyl cellulose, glycerin, poloxamer, meglumine, iron oxide and magnesium stearate. Raw materials and accessories for the tablet are safe and easily available; the prepared tablet has good dissolvability and a good dissolution rate and enables stable plasma concentration; prepared repaglinide tablets have the function characteristics of rapid absorption, fast action, a fast clearance speed in vivo and a short half life and canbe used for treating 2 type diabetes. Prescription for the repaglinide cystals is reasonable; the repaglinide cystals have stable and reliable quality and good disintegration time and dissolution rates; repaglinide tablets are prepared through a direct compression process, which enables a simple process, a short production period and low production cost; therefore, industrial production of the repaglinide tablets is easy to realize.

Description

Technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a repaglinide crystal, a preparation method thereof and a solid oral preparation containing the crystal. Background technique [0002] Repaglinide, English name: repaglinide, its chemical name: S(+)-2-ethoxy-4-{2-[(3-methyl-1-(2-(1-piperidinyl) Phenyl)butyl)amino]-2-oxoethyl}benzoic acid, molecular formula: C 27 H 36 N 2 O 4 , Molecular weight: 452.6, structural formula is as follows: [0003] [0004] Repaglinide is a white or yellowish-white powder at room temperature. It is a new type of short-acting oral insulin secretion-promoting and hypoglycemic agent with amino acid structure and non-sulfonylurea. Developed by (German) Boehringer Ingelheim, developed by Novo Nordisk and listed in the United States for the first time in April 1998, and listed in the United Kingdom in October of the same year. Repaglinide stimulates the pancreas to release insulin to rapidly reduce b...

Claims

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Application Information

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IPC IPC(8): C07D295/135A61K31/451A61K9/20A61P3/10
Inventor 马鹰军王小树钟正明罗韬
Owner HAINAN JINRUI PHARMA
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